Erigeron breviscapus is a flowering plant native to southwest China that has been used in traditional Chinese medicine for thousands of years. It contains bioactive compounds including breviscapine, which is 85% scutellarin. Studies show breviscapine and its constituents have benefits for cardiovascular and cerebrovascular diseases by protecting endothelial cells, dilating blood vessels, and reducing inflammation. Clinical trials indicate breviscapine may improve outcomes for conditions like angina and diabetic nephropathy when combined with conventional therapies, but more high-quality research is still needed to confirm its efficacy and safety.

1. FLOWER AS MEDICINE:
DAISY
ERIGERON BREVISCAPUS
By
Kevin KF Ng, MD, PhD.
Former Associate Professor of Medicine
Division of Clinical Pharmacology
University of Miami, Miami, FL, USA
Email: kevinng68@gmail.com
A Slide Presentation for HealthCare Provider Seminar Oct. 2019

2. Outline of Lecture: Daisy flower
▪ What is Erigeron breviscapus?
▪ Historical milestones
▪ Source of daisy flowers.
▪ Bioactive compounds
▪ Pharmacokinetics
▪ Heath benefits
▪ Use, side effects and toxicity
▪ Clinical studies and meta-analysis
▪ Summary

3. Erigeron breviscapus : Flora of China
▪Erigeron breviscapus
(Vaniot) Handel-Mazzetti, Symb. Sin. 7: 1093. 1936.
▪短葶飞蓬 duan ting fei peng
http://www.efloras.org/florataxon.aspx?flora_id=2&taxon_id=200023890

4. 6 Provinces in China where Erigeron breviscapus is cultivated
https://irp-cdn.multiscreensite.com/fa269471/files/uploaded/Breviscapine%20Feb%202019.pdf

5. What is Erigeron breviscapus ?
▪ Erigeron breviscapus is a Chines species of flowering plants
in the daisy family.
▪ It is found only in China, in the provinces of Guangxi,
Guizhou, Hunan, Sichuan, Tibet and Yunnan.
▪ It is a perennial herb growing up to 20 inches high.
▪ Its flower heads have blue, purple or white ray florets
surrounding yellow disc florets.
▪ It is a Traditional Chinese Medicine used as a
microcirculation promoter in stroke and cardiovascular
disease.
https://en.wikipedia.org/wiki/Erigeron_breviscapinus

6. Historical milestones of Daisy Flower (Erigeron breviscapus)

7. Scientific Classification of Daisy flower (erigeron breviscapus)

8. Erigeron breviscapus (A) whole plant and (B) flower
https://pdfs.semanticscholar.org/aea9/28c567c77917d8d70a8f30ff86eafc5e
4e8c.pdf?_ga=2.23870073.231108289.1563251047-964379817.1563251047

9. Anatomy of a daisy flower (Erigeron breviscapus)
disc florets
Ray florets
a daisy flower close-up

10. Isolation of bioactive compounds from Erigeron breviscapus
Flower Flower Extract
Breviscapine
(Total flavonoids)

11. Solubility of Bioactive Breviscapine
▪ Soluble in
▪ methanol
▪ pyridine
▪ dilute alkali solution
▪ Slightly soluble in
▪ hot water
▪ ethanol
▪ ethyl acetate
▪ Almost insoluble in
▪ water
▪ ether
▪ chloroform
▪ benzene
https://www.ingredientsonline.com/breviscapine-scutellarin-pkg122.html

12. Isolation of bioactive compounds from Erigeron breviscapus
Flower Extract
Breviscapine
(Total flavonoids)
Scutellarin
85%
Apigenin
Scutellarin
85%
minor
constituents
Scutellarin

13. Chemical constituents from flowers of Erigeron breviscapus
[Article in Chinese] 2011
Twelve compounds were isolated and structurally identified as :
1. quercetin-3-O-beta-D-glucoside (1),
2. 5, 7-dihydroxychromone (2),
3. 3-O-caffeoyl-gamma-quinide (3),
4. naringenin (4),
5. 3, 5-di-O-caffeoylquinic acid (5),
6. 3,4-di-O-caffeoylquinic acid (6),
7. 4, 5-di-O-caffeoylquinic acid (7),
8. 1,3-di-O-caffeoylquinic acid (8),
9. 1, 5-di-O-caffeoylquinic acid (9),
10. 3-O-caffeoylquinic acid (10),
11. 4-O-caffeoylquinic acid (11)
12. chlorogenic acid (12).
https://www.ncbi.nlm.nih.gov/pubmed/22779177

14. Major bioactive compounds of breviscapine (2013)
▪ Scutellarin
▪ 1,5-dicaffeoylquinic acid
▪ 3,5-dicaffeoylquinic acid
▪ erigoster B.
https://www.researchgate.net/figure/The-concentrations-of-four-chemical-
compounds-in-23-E-breviscapus-populations_fig5_258825840

15. Number of publications on erigeron breviscapus (Daisy flower)
in PubMed from 1980 to 2019
https://www.ncbi.nlm.nih.gov/pubmed/?term=erigeron+breviscapus

16. Number of publications on scutellarin and apigenin in PubMed from
1992 to 2018
https://www.ncbi.nlm.nih.gov/pubmed/?term=scutellarin

17. Current usage of breviscapine in China
▪ The plant Erigeron breviscapus has been used as a Traditional
Chinese Medicine for thousands of years.
▪ About 10 million patients are now being treated yearly with
breviscapine for cerebrovascular and cardiovascular diseases.
▪ Breviscapine is approved as a prescription drug in China.
▪ Demand for breviscapine is much greater than supply.
▪ Attempts were made to synthesize breviscapine by yeast.
▪ The product breviscapine contains mostly scutellarin with little
apigenin.

18. https://www.asianscientist.com/2011/06/pharma/sihuan-pharma-vinise-pharma-tcm/

19. Oral bioavailability of scutellarin in rat (2005)
▪ Oral bioavailability 10.67%±4.78%
https://link.springer.com/article/10.1007/BF03190615

20. Parmacoknetics parameters for scutellarin after oral administration
in male and female rats (mean±SD, n=10). (2011)
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4002508/

21. Pharmacokinetics and metabolism of the flavonoid scutellarin
in humans after a single oral administration. (2006)
https://www.ncbi.nlm.nih.gov/pubmed/16714374

22. Isolation and identification of ten metabolites of breviscapine in
rat urine. (2007)
The ten metabolites were identified as :
1. scutellarein-6,7-di-O-beta-D-glucuronide
2. scutellarein
3. 6-O-methyl-scutellarin
4. 6-O-methyl-scutellarein
5. scutellarein-6-O-beta-D-glucuronide
6. scutellarein-5-O-beta-D-glucuronide
7. scutellarin
8. scutellarein-7-O-sulfate
9. apigenin-5-O-beta-D-glucuronide
10. apigenin-4'-O-beta-D-glucuronide
https://www.jstage.jst.go.jp/article/bpb/30/7/30_7_1308/_pdf/-char/en

23. Traditional use of Daisy flower (Erigeron breviscapus)
since 1436 in China
Ischemic disease
of the
Heart
Brain
Human

24. Modern scientific studies of Daisy flower
(Erigeron breviscapus) in China last 30 years
Colon cancer
Lung
Liver
Tongue
Lymphoma
Coronary heart disease
Myocardial infarction
Arrhythmia
Hypertension
Viral myocarditis
Chronic heart failure
Pulmonary heart disease
Cerebrovascular disease
Diabetic kidney disease
Cell lines Animals Human
Breviscapine is now officially designated as a prescription drug in China
Anti-cancer
Anti-thrombosis
Anti-coagulation

25. Therapeutic Effects of Breviscapine in Cardiovascular Diseases:
A Review (2017)
Cells/tissue
In vitro
• Myocardial protection
• Smooth muscle
protection
• Antiarrhythmic effect
• Vasodilating effect
Animal
In vivo
• Myocardial protection
• Heart failure
• Lipid lowering
• Erectile function
Human
clinical trials
• Stable angina
• Unstable angina
• Myocardial infarction
• Hypertension
• Cerebral haemorrhage
• Atrial fibrillation
• Pulmonary heart
disease
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5441392/

26. Major bioactive compounds of breviscapine and their health benefits
BenefitFlavonoidExtract
Breviscapine
Scutellarin
Cardiovascular
disease
Cerebrovascular
disease
Apigenin
Anti-
inflammatory
80-90%

27. Health benefits of Bioactive compounds in
Erigeron breviscapus
Adapted from https://www.mskcc.org/cancer-
care/integrative-medicine/herbs/cinnamon

28. Protective effects of scutellarin and breviscapine on brain and
heart ischemia in rats (2007)
https://www.ncbi.nlm.nih.gov/pubmed/17878763

29. Scutellarin protects against vascular endothelial dysfunction
and prevents atherosclerosis via antioxidation (2018)
https://www.ncbi.nlm.nih.gov/pubmed/29655699

30. Scientific studies of Apigenin on cell lines, animals and human.

31. Neuroprotective Effect of Scutellarin on Ischemic Cerebral Injury by
Down-Regulating the Expression of Angiotensin-Converting Enzyme
and AT1 Receptor (2016)
▪ Scutellarin decreased the following changes in ischemic brains:
▪ neurological deficit score,
▪ infarct area,
▪ cell apoptosis and
▪ morphological changes
▪ ACE and AT1R expression
▪ Ang II, TNF-α, IL-6, and IL-1β
▪ Scutellarin has a potent ACE inhibitor activity.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5441392/
Scutellarin

32. Neuroprotective Effect of Scutellarin on Ischemic Cerebral Injury by
Down-Regulating the Expression of Angiotensin-Converting Enzyme
and AT1 Receptor (2016)
https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0146197

33. Therapeutic Effects of Breviscapine in Cardiovascular Diseases:
A Review (2007)
▪ Endothelial Protective Effect
▪ Vasodilating Effect
▪ Protective Effect against Ischemia/Reperfusion
▪ Improving Erectile Dysfunction
▪ Anti-inflammatory Effect
▪ Anticoagulation Effect
▪ Antithrombotic Effect
▪ Myocardial Protective Effect
▪ Reduction of Smooth Muscle Cell Migration and Proliferation
▪ Antiarrhythmic Effect
▪ Lipid-Lowering Effect
https://pdfs.semanticscholar.org/aea9/28c567c77917d8d70a8f30ff86eafc5e4e8c.p
df?_ga=2.23870073.231108289.1563251047-964379817.1563251047
Breviscapine molecule structure

34. Novel anti-obesity effect of scutellarin and potential underlying
mechanism of actions. (2019)
https://www.ncbi.nlm.nih.gov/pubmed/31228804

35. Current usage of Breviscapine
▪ Medicinal properties:
▪ Breviscapine is a prescription drug in China
▪ Microvascular promotor
▪ Functional food:
▪ Nutritional bar
▪ Smoothie
▪ Yogurt
▪ Dietary supplements:
▪ Powder
▪ Tablets
▪ Capsules
▪ Softgels

36. What is meta-analysis: evidence-based medicine
https://rdfeinman.files.wordpress.com/2015/08/meta-anal_whatis.png

37. Meta-analysis: Hierarchy of evidence in clinical studies
use of statistical methods to summarise the results of these studies.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3049418/

38. Breviscapine plus Western Medicine improve the
symptoms and EKG changes of
patients with angina pectoris
https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0129969

39. Breviscapine improves the 24-h urine protein in
patients with diabetic nephropathy. (2016)
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4998064/

40. Breviscapine improves blood urea nitrogen in
patients with diabetic nephropathy. (2016)
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4998064/

41. Breviscapine improves serum creatinine in
patients with diabetic nephropathy (2016)
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4998064/

42. Breviscapine lowers cholesterol in patients with diabetic
nephropathy (2006)
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4998064/

43. Breviscapine lowers triglyceride in patients with
diabetic nephropathy. (2017)
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4998064/

44. Effect of breviscapine on high density lipoproteins in
patients with diabetic nephropathy. (2017)
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4998064/

45. Effect of breviscapine injection on diabetic nephropathy:
A meta-analysis of randomized controlled trials. (2016)
▪ A total of 29 studies containing 37 trials were included.
▪ There were 2,097 patients, 1,054 cases in test groups and 1,043
cases in control groups.
▪ All clinical studies showed low overall quality.
▪ The evidences suggest that the combination of Breviscapine
Injection and conventional therapy were better in the treatment of
diabetic neuropathy, especially in stages Ⅲ and Ⅳ.
▪ The safety of Breviscapine Injection needs to be further explored.
▪ Further studies are warranted to establish its efficacy and safety.
https://www.ncbi.nlm.nih.gov/pubmed/30989899

46. Efficacy and safety of breviscapine injection in treatment of
unstable angina pectoris: systematic review and Meta-analysis (2018)
▪ A total of 36 studies involving 3,058 patients were examined.
▪ There were1,552 cases in the trial group, 1,506 cases in the
control group; 1,846 males and, 1,212 females.
▪ All clinical studies showed low quality.
▪ The combination of breviscapine injection and conventional
therapy appeared to be superior to conventional therapy in
angina pectoris.
▪ Due to the low quality of the study it is necessary to design
high-quality, multi-center randomized double-blind controlled
trials to determine its efficacy and safety.
https://www.ncbi.nlm.nih.gov/pubmed/30453722

47. Summary
▪ Erigeron breviscapus is a flowering plant belonging to the daisy family.
▪ It is grown only in southwest regions of China.
▪ It has been used as a Traditional Chines Medicine for thousands of years.
▪ The demand for breviscapine, the flavonoid extract of the plant, led to the
synthesis of the compound in 2018.
▪ Breviscapine contains 85% of scutellarin and small amount of apigenin.
▪ The oral bioavailability of scutellarin is about 10% with a half-life of about 6 hr.
▪ Much studies have been done in ischemic diseases of the brain and the heart.
▪ The efficacy and safety of breviscapine and scutellarin have yet to be
established.

48. ANY QUESTION?
Please contact
Kevin KF Ng, MD, PhD
Email: kevinng68@gmail.com